超滤质谱技术在药物小分子与生物靶分子相互作用研究中的应用

Applications of Ultrafiltration Mass Spectrometry in the Studies on Interaction Between Small Drug Molecule and Biological Target

药物小分子与生物体内靶分子之间的相互作用,是药物发挥其药理活性的重要途径之一。因此,高通量地筛选出能够与生物靶分子相互作用且具有生物活性的药物小分子,对于新药开发研究具有重要的理论意义和实际应用价值。超滤质谱技术是超滤装置与质谱技术结合后形成的一种新的分析方法,它能够在液相条件下快速识别并鉴定出与生物靶分子结合的药物小分子配体。与其他分析方法相比,超滤质谱技术具有快速、灵敏、高通量的特点,因而被广泛应用于研究药物小分子和生物靶分子相互作用。本文综述了超滤质谱技术的原理、特点和实验操作中的一些关键问题。重点介绍了超滤质谱技术在药物小分子与生物靶分子相互作用研究中的应用进展,并对其未来的发展方向进行了展望。

The interaction between small drug molecule and biological target in vivo is one of the most important factors that determine the therapeutic activity of the medicine.Screening small drug molecule that can bind with biological target and show well pharmacological effects will promote the development of new medicine discovery significantly.Several approaches have been developed to screening of combinatorial libraries and natural product extracts for biologically active compounds.Ultrafiltration mass spectrometry is a combination of ultrafiltration equipment and mass spectrometry,which is a valuable approach for the selection,structure analysis,and identification of low molecular weight compounds that interact with biological targets in the solution phase.It has been developed as a powerful tool for the determination of the interaction between small drug molecule and biological target because of its high speed,high sensitivity,and its high throughput screening ability.In this paper,the fundamental principles on which the ultrafiltration mass spectrometry is based,and the experimental details that must be considered during the operation of ultrafiltration equipment are introduced.The developments and applications of the ultrafiltration mass spectrometry in the studies on the interaction between small drug molecule and biological target are reviewed.In addition,the development trend of the ultrafiltration mass spectrometry are also discussed.